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Article ; Online: Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs

Ashraf A. Aly / Alaa A. Hassan / Maysa M. Makhlouf / Stefan Bräse

Molecules, Vol 25, Iss 3036, p

2020 Volume 3036

Abstract: Mercapto-substituted 1,2,4-triazoles are very interesting compounds as they play an important role in chemopreventive and chemotherapeutic effects on cancer. In recent decades, literature has been enriched with sulfur- and nitrogen-containing ... ...

Abstract	Mercapto-substituted 1,2,4-triazoles are very interesting compounds as they play an important role in chemopreventive and chemotherapeutic effects on cancer. In recent decades, literature has been enriched with sulfur- and nitrogen-containing heterocycles which are used as a basic nucleus of different heterocyclic compounds with various biological applications in medicine and also occupy a huge part of natural products. Therefore, we shed, herein, more light on the synthesis of this interesting class and its application as a biologically active moiety. They might also be suitable as antiviral and anti-infective drugs.
Keywords	1,2,4-triazole ring ; synthesis ; reactions ; biological activity ; Organic chemistry ; QD241-441
Language	English
Publishing date	2020-07-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Chemistry of Substituted Thiazinanes and Their Derivatives

Alaa A. Hassan / Stefan Bräse / Ashraf A. Aly / Hendawy N. Tawfeek

Molecules, Vol 25, Iss 5610, p

2020 Volume 5610

Abstract: Thiazinanes and its isomeric forms represent one of the most important heterocyclic compounds, and their derivatives represented a highly potent drug in disease treatment such as, 1,1-dioxido-1,2-thiazinan-1,6-naphthyridine, which has been shown to have ... ...

Abstract	Thiazinanes and its isomeric forms represent one of the most important heterocyclic compounds, and their derivatives represented a highly potent drug in disease treatment such as, 1,1-dioxido-1,2-thiazinan-1,6-naphthyridine, which has been shown to have anti-HIV activity by a mechanism that should work as anti-AIDS treatment, while ( Z )-methyl 3-(naphthalen-1-ylimino)- 2-thia-4-azaspiro[5 5]undecane-4-carbodithioate showed analgesic activity, cephradine was used as antibiotic and chlormezanone was utilized as anticoagulants. All publications were interested in the chemistry of thiazine (partially or fully unsaturated heterocyclic six-membered ring containing nitrogen and sulfur), but no one was dealing with thiazinane itself which encouraged us to shed new light on these interesting heterocycles. This review was focused on the synthetic approaches of thiazinane derivatives and their chemical reactivity.
Keywords	biologic activity ; fused-heterocycles ; spiro compounds ; structures ; thiazinanes ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2020-11-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis and Antiproliferative Potential of Thiazole and 4-Thiazolidinone Containing Motifs as Dual Inhibitors of EGFR and BRAF V600E

Alaa A. Hassan / Nasr K. Mohamed / Ashraf A. Aly / Mohamed Ramadan / Hesham A. M. Gomaa / Ahmed T. Abdel-Aziz / Bahaa G. M. Youssif / Stefan Bräse / Olaf Fuhr

Molecules, Vol 28, Iss 24, p

2023 Volume 7951

Abstract: Thiazole and thiazolidinone recur in a wide range of biologically active compounds that reach different targets within the context of tumors and represent a promising starting point to access potential candidates for treating metastatic cancer. Therefore, ...

Abstract	Thiazole and thiazolidinone recur in a wide range of biologically active compounds that reach different targets within the context of tumors and represent a promising starting point to access potential candidates for treating metastatic cancer. Therefore, searching for new lead compounds that show the highest anticancer potency with the fewest adverse effects is a major drug-discovery challenge. Because the thiazole ring is present in dasatinib, which is currently used in anticancer therapy, it is important to highlight the ring. In this study, cycloalkylidenehydrazinecarbothioamides (cyclopentyl, cyclohexyl, cyclooctyl, dihydronapthalenylidene, flurine-9-ylidene, and indolinonyl) reacted with 2-bromoacetophenone and diethylacetylenedicarboxylate to yield thiazole and 4-thiazolidinone derivatives. The structure of the products was confirmed by using infrared (IR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry, and single-crystal X-ray analyses. The antiproliferative activity of the newly synthesized compounds was evaluated. The most effective inhibitory compounds were further tested in vitro against both epidermal growth factor receptor (EGFR) and B-Raf proto-oncogene, serine/threonine kinase (BRAF V600E ) targets. Additionally, molecular docking analysis examined how these molecules bind to the active sites of EGFR and BRAF V600E .
Keywords	thiazole ; 4-thiazolidinone ; EGFR ; BRAF ; dual inhibitors ; anticancer ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2023-12-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Crystal structure of (E)-1-(3-benzyl-5-phenyl-1,3-thiazol-2-ylidene)-2-[(E)-1,2,3,4-tetrahydronaphthalen-1-ylidene]hydrazin-1-ium bromide

Shaaban K. Mohamed / Sahar M. I. Elgarhy / Alaa A. Hassan / Güneş Demirtaş / Joel. T. Mague / Youssef Ramli

Acta Crystallographica Section E: Crystallographic Communications, Vol 77, Iss 4, Pp 420-

2021 Volume 423

Abstract: In the title molecular salt, C26H24N3S+·Br−, the dihedral angles between the thiazole ring and its attached phenyl and benzoyl rings are 54.81 (7) and 85.51 (7)°, respectively. In the crystal, ion pairs are linked by C—H.Br and N—H.Br hydrogen bonds and ... ...

Abstract	In the title molecular salt, C26H24N3S+·Br−, the dihedral angles between the thiazole ring and its attached phenyl and benzoyl rings are 54.81 (7) and 85.51 (7)°, respectively. In the crystal, ion pairs are linked by C—H.Br and N—H.Br hydrogen bonds and are connected into helical chains extending along the c-axis direction by weak, electrostatic S.Br− interactions. A Hirshfeld surface analysis was performed, which showed the dominant role of H.H contacts (51.3%).
Keywords	crystal structure ; dihydronaphthalene ; thiazole ; hydrazinium salt ; hydrogen bond ; Chemistry ; QD1-999
Language	English
Publishing date	2021-04-01T00:00:00Z
Publisher	International Union of Crystallography
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis of novel amidines via one-pot three component reactions

Essmat M. El-Sheref / Hendawy N. Tawfeek / Alaa A. Hassan / S. Bräse / Mohammed A. I. Elbastawesy / Hesham A. M. Gomaa / Yaser A. Mostafa / Bahaa G. M. Youssif

Frontiers in Chemistry, Vol

Selective topoisomerase I inhibitors with antiproliferative properties

2022 Volume 10

Abstract: Novel series of amidines were synthesized via the interaction between alicyclic amines, cyclic ketones, and a highly electrophilic 4-azidoquinolin-2(1H)-ones without any catalyst or additive. All the obtained products were elucidated based on NMR ... ...

Abstract	Novel series of amidines were synthesized via the interaction between alicyclic amines, cyclic ketones, and a highly electrophilic 4-azidoquinolin-2(1H)-ones without any catalyst or additive. All the obtained products were elucidated based on NMR spectroscopy, mass spectrometry, and elemental analysis. The reaction conditions were optimized using cyclohexanone (2), piperidine (3a), and 4-azido-quinolin-2(1H)-one (1a) under an air atmosphere. The new compounds 4a-l and 5a-c were tested for antiproliferative activity against four cancer cell lines using doxorubicin as a reference drug. The most potent derivatives were compounds 4b, 4d, 4e, 4i, and 5c, with GI50 ranging from 1.00 µM to 1.50 µM. Compound 5c was the most effective derivative against the four cancer cell lines, outperforming doxorubicin. The compounds 4b, 4d, 4e, 4i, and 5c were studied further as topoisomerase I and IIα inhibitors. The compounds tested showed selective inhibition of topo I over topo IIα. Finally, docking studies explain why these compounds prefer topo I over topo IIα.
Keywords	one-pot 3CR ; 4-azido-quinolin-2(1H)-ones ; topo ; antiproliferative ; viability ; heterocycles ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2022-11-01T00:00:00Z
Publisher	Frontiers Media S.A.
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Autoxidation of 4-Hydrazinylquinolin-2(1 H )-one; Synthesis of Pyridazino[4,3- c :5,6- c ′]diquinoline-6,7(5 H ,8 H )-diones

Sara M. Mostafa / Ashraf A. Aly / Alaa A. Hassan / Esraa M. Osman / Stefan Bräse / Martin Nieger / Mahmoud A. A. Ibrahim / Asmaa H. Mohamed

Molecules, Vol 27, Iss 2125, p

2022 Volume 2125

Abstract: An efficient synthesis of a series of pyridazino[4,3- c :5,6- c ′]diquinolines was achieved via the autoxidation of 4-hydrazinylquinolin-2(1 H )-ones. IR, NMR ( 1 H and 13 C), mass spectral data, and elemental analysis were used to fit and elucidate the ... ...

Abstract	An efficient synthesis of a series of pyridazino[4,3- c :5,6- c ′]diquinolines was achieved via the autoxidation of 4-hydrazinylquinolin-2(1 H )-ones. IR, NMR ( 1 H and 13 C), mass spectral data, and elemental analysis were used to fit and elucidate the structures of the newly synthesized compounds. X-ray structure analysis and theoretical calculations unequivocally proved the formation of the structure. The possible mechanism for the reaction is also discussed.
Keywords	4-hydrazinylquinolin-2(1 H )-one ; pyridazino[4,3- c :5,6- c ′]diquinoline-6,7(5 H ,8 H )-dione ; autoxidation reaction ; X-ray ; DFT ; Organic chemistry ; QD241-441
Language	English
Publishing date	2022-03-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis of New Planar-Chiral Linked [2.2]Paracyclophanes- N -([2.2]-Paracyclophanylcarbamoyl)-4-([2.2]Paracyclophanylcarboxamide, [2.2]Paracyclophanyl-Substituted Triazolthiones and -Substituted Oxadiazoles

Ashraf A. Aly / Stefan Bräse / Alaa A. Hassan / Nasr K. Mohamed / Lamiaa E. Abd El-Haleem / Martin Nieger

Molecules, Vol 25, Iss 3315, p

2020 Volume 3315

Abstract: The manuscript describes the synthesis of new racemic and chiral linked paracyclophane assigned as N -5-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)carbamoyl)-5’-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)carboxamide. The procedure depends upon the reaction ...

Abstract	The manuscript describes the synthesis of new racemic and chiral linked paracyclophane assigned as N -5-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)carbamoyl)-5’-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)carboxamide. The procedure depends upon the reaction of 5-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)hydrazide with 5-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)isocyanate. To prepare the homochiral linked paracyclophane of a compound, the enantioselectivity of 5-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)carbaldehyde (enantiomeric purity 60% ee), was oxidized to the corresponding acid, which on chlorination, gave the corresponding acid chloride of [2.2]paracyclophane. Following up on the same procedure applied for the preparation of racemic-carbamoyl and purified by HPLC purification, we succeeded to obtain the target Sp - Sp - N -5-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)carbamoyl)-5’-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)carboxamide. Subjecting N -5-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)hydrazide to various isothiocyanates, the corresponding paracyclophanyl-acylthiosemicarbazides were obtained. The latter compounds were then cyclized to a new series of 5-(1,4(1,4)-dibenzenacyclohexaphane-1 2 -yl)-2,4-dihydro-3 H -1,2,4-triazol-3-thiones. 5-(1,4(1,4)-Dibenzenacyclohexaphane-1 2 -yl)-1,3,4-oxadiazol-2-amines were also synthesized in good yields via internal cyclization of the same paracyclophanyl-acylthiosemicarbazides. NMR, IR, and mass spectra (HRMS) were used to elucidate the structure of the obtained products. The X-ray structure analysis was also used as an unambiguous tool to elucidate the structure of the products.
Keywords	HPLC ; chiral N -([2.2]-paracyclophanylcarbamoyl)-4-([2.2] paracyclophanylcarboxamide ; hydrazinecarbothioamide-paracyclophanes ; paracyclophanyl-1,2,4-triazol-3-thione ; paracyclophanyl)-1,3,4-oxadiazoles ; Organic chemistry ; QD241-441
Subject code	333
Language	English
Publishing date	2020-07-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Formation of thiadiazole, thiadiazine, thiadiazepine and pyrazole derivatives in the reaction of 2,4-disubstituted thiosemicarbazides with tetracyanoethylene

Alaa A. Hassan / Ashraf A. Aly / Sara M. Mostafa / Dietrich Döpp

ARKIVOC, Vol 2018, Iss 3, Pp 200-

2018 Volume 211

Keywords	Organic chemistry ; QD241-441
Language	English
Publishing date	2018-03-01T00:00:00Z
Publisher	Arkat USA, Inc.
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: A convenient and efficient synthesis of thiazolidin-4-ones via cyclization of substituted hydrazinecarbothioamides

Alaa A. Hassan / Nasr K. Mohamed / Kamal M.A. El-Shaieb / Hendawy N. Tawfeek / Stefan Bräse / Martin Nieger

Arabian Journal of Chemistry, Vol 12, Iss 2, Pp 289-

2019 Volume 294

Abstract: 2-Substituted hydrazinecarbothioamides and N,2-disubstituted hydrazinecarbothioamides react in high yield with dimethyl acetylenedicarboxylate (DMAD) to give 4-oxo-Z-(thiazolidin-5-ylidene) acetate derivatives. Several mechanistic options involving ... ...

Abstract	2-Substituted hydrazinecarbothioamides and N,2-disubstituted hydrazinecarbothioamides react in high yield with dimethyl acetylenedicarboxylate (DMAD) to give 4-oxo-Z-(thiazolidin-5-ylidene) acetate derivatives. Several mechanistic options involving interaction are presented. The structures of thiazolidin-4-ones have been unambiguously confirmed by single crystal X-ray crystallography. Keywords: Hydrazinecarbothioamides, Dimethyl acetylenedicarboxylate, Thiazolidin-4-ones, X-ray crystallography
Keywords	Chemistry ; QD1-999
Language	English
Publishing date	2019-02-01T00:00:00Z
Publisher	Elsevier
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: New Paracyclophanylthiazoles with Anti-Leukemia Activity

Ashraf A Aly / Stefan Bräse / Alaa A. Hassan / Nasr K. Mohamed / Lamiaa E. Abd El-Haleem / Martin Nieger / Nesrin M. Morsy / Elshimaa M. N. Abdelhafez

Molecules, Vol 25, Iss 3089, p

Design, Synthesis, Molecular Docking, and Mechanistic Studies

2020 Volume 3089

Abstract: A new series of methyl 2-(2-(4′-[2.2]paracyclophanyl)-hydrazinylidene)-3-substituted-4-oxothiazolidin-5-ylidene)acetates 3a – f were synthesized from the reaction of paracyclophanyl-acylthiosemicarbazides 2a – f with dimethyl acetylenedicarboxylate. ... ...

Abstract	A new series of methyl 2-(2-(4′-[2.2]paracyclophanyl)-hydrazinylidene)-3-substituted-4-oxothiazolidin-5-ylidene)acetates 3a – f were synthesized from the reaction of paracyclophanyl-acylthiosemicarbazides 2a – f with dimethyl acetylenedicarboxylate. Based upon nuclear magnetic resonance (NMR), infrared (IR), and mass spectra (HRMS), the structure of the obtained products was elucidated. X-ray structure analysis was also used as unambiguous tool to elucidate the structure of the products. The target compounds 3a – f were screened against 60 cancer cell lines. They displayed anticancer activity against a leukemia subpanel, namely, RPMI-8226 and SR cell lines. The activity of compound 3a was found as the most cytotoxic potency against 60 cancer cell lines. Consequently, it was selected for further five doses analysis according to National Cancer Institute (NCI) protocol. The cytotoxic effect showed selectivity ratios ranging between 0.63 and 1.28 and between 0.58 and 5.89 at the GI 50 and total growth inhibition (TGI) levels, respectively. Accordingly, compound 3a underwent further mechanistic study against the most sensitive leukemia RPMI-8226 and SR cell lines. It showed antiproliferation with IC50 = 1.61 ± 0.04 and 1.11 ± 0.03 µM against RPMI-8226 and SR cell lines, respectively. It also revealed a remarkable tubulin inhibitory activity, compared to colchicine with IC50 = 4.97 µM/mL. Caspase-3, BAX, and Bcl-2 assays for 3a using annexin V-FITC staining revealed significant pro-apoptotic activity. Furthermore, multidrug-resistant leukemia SR cells were used to show better resistance indices (1.285 ng/mL, 1.15-fold) than the reference. Docking studies with β-tubulin indicate that most of the tested compounds illustrated good binding at the colchicine binding site of the enzyme, especially for compound 3a , which made several interactions better than that of the reference colchicine.
Keywords	paracyclophanes ; NMR ; X-ray ; NCI-60 ; cancer cell lines ; mechanism ; Organic chemistry ; QD241-441
Subject code	500
Language	English
Publishing date	2020-07-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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