- Synthesis and Antiproliferative Activity of Novel Hydrazono Thiazolidene and Thiazole Derivatives Bearing Rhodanine Moiety
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Abstract: Some new fluoro-heterocyclic compounds containing thiazole and pyridine moities have been synthesized and studied for their antiproliferative activity. Thiazole derivatives have been synthesized by the reaction of alpha-halo carbonyl compounds with thiosemicarbazones. Some pyridine derivatives have been synthesized by the reaction of chalcone with cyanothioacetamide and/or malononitrile. Spectroscopic methods have been used for elucidating molecular structures of the products. Cytotoxic activity of several derivatives has been tested against human breast cancer (MCF-7), human colon cancer (HCT-116) and human liver cancer (Hep-G2) by the SRB method. Most of compounds exhibit mild effect on the tested cell lines. One of thiazolidin-4-one derivatives has been characterized by moderate to strong effect on MCF-7 cell line.
- Amr, A. E.,Azab, M. E.,Elasasy, M. E. A.,Elnaggar, D. H.,Hafez, N. A. Abdel,Mohamed, A. M.,Omran, M. M.
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p. 915 - 925
(2021/06/26)
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- Oxime ether compound and application thereof
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The invention discloses an oxime ether compound with a novel structure, the structure is shown as a general formula I, and the definition of each substituent group in the formula is shown in the specification. The compound shown in the general formula I h
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Paragraph 0192-0194
(2021/05/12)
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- Design, synthesis and molecular docking studies of some thiazole clubbed heterocyclic compounds as possible anti-infective agents
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The present work describes synthesis of a series of 5-((1-(4-(4-chlorophenyl)thiazol-2-yl)-3- aryl-1H-pyrazol-4-yl)methylene)-2-(arylimino)thiazolidin-4-one derivatives and their molecular docking and biological evaluation as possible antimalarial, anthelmintic and antimicrobial agents. The synthesis of compounds has been accomplished by adopting suitable synthetic methods. Structures of newly synthesized compounds were characterized and authenticated by spectral methods such as IR, 1H-NMR and mass spectra. Synthesized compounds were screened for their in vitro antimicrobial activity against selected bacterial strains and fungal strains viz. B. subtilis, S. aureus, E. coli, P. fluorescens, C. albicans, C. glabrata and antimalarial studies against P. falciparum. Titled compounds were also tested against Pheretima posthuma (earthworm) for their anthelmintic activity. Molecular docking was done to study the binding modes of the potent compounds against Escherichia coli (PDB ID: 1AB4) and Candida P450DM (PDB ID: 1EA1) enzymes. The results revealed that all the compounds exhibited moderate to significant antimicrobial activities. Antimalarial activity screening revealed that one compound 8i showed significant antimalarial activity with of IC50; 0.59 μg/mL as compared to standard drugs chloroquine (IC50= 0.020 μg/mL) and quinine (IC50; 0.268 μg/mL). The most active compound exhibited the mean paralysis time of 19.2 ± 0.9 min and mean death time of 31.7 ± 2.5 min. It can be concluded that some of the synthesized compounds have remarkable antiinfective, antimalarial and anthelmintic activity and are suitable candidates for further scientific exploration.
- Sharma, Prabodh Chander,Saini, Anil,Bansal, Kushal Kumar,Sharma, Archana,Gupta, Girish Kumar
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p. 716 - 726
(2018/07/13)
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- Novel thiazole clubbed triazole derivatives as antimicrobial, antimalarial, and cytotoxic agents
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Thiazole is one of the most potential heterocyclic moieties in bioorganic chemistry and is major tool in drug design and discovery. The present work describes the synthesis of a series of N-{(1-(4-(4bromophenyl) thiazol-2-yl)-3-substitutedphenyl-1H-pyrazo
- Bansal, Kushal K.,Sharma, Diksha,Sharma, Archana,Rajak, Harish,Sharma, Prabodh C.
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p. 305 - 312
(2018/09/14)
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- In vitro and in silico antimalarial activity of 2-(2-hydrazinyl)thiazole derivatives
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A series of 2-(2-hydrazinyl)thiazole derivatives with a wide range of substitutions at 2-, 4- and 5-positions were synthesized, characterized and evaluated their inhibitory potentials against plasmodium falciparum, NF54, by in vitro blood stage assay. The compounds, ethyl-4-methyl-2-[(E)-2-[1-(pyridin-2- yl)ethylidene]hydrazin-1-yl]-1,3-thiazole-5-carboxylate, 4d, and 1-{4-methyl-2-[(E)-2-[1-(pyridin-2-yl)ethylidene]hydrazin-1-yl]-1, 3-thiazol-5-yl}ethan-1-one, 5d showed significant antimalarial activity with IC50 values of 0.725 μM and 0.648 μM respectively. To understand the mechanism, the binding interactions between 2-(2-hydrazinyl) thiazole derivatives and trans-2-enoyl acyl carrier protein reductase of P. falciparum were studied through docking studies. The half maximal inhibitory concentration (IC50) through docking studies for the compounds, 4d and 5d were found to be 22.88 μM and 631.84 μM respectively.
- Makam, Parameshwar,Thakur, Prasoon Kumar,Kannan, Tharanikkarasu
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p. 138 - 145
(2014/01/06)
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- Some new organotin(IV) complexes of biologically important semicarbazones and thiosemicarbazones
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The present paper is a report on the synthesis of some new organotin(IV) complexes by the reactions of bis(tributyltin)oxide and semicarbazones/ thiosemicarbazones using benzene as reaction medium. Semicarbazones and thiosemicarbazones are prepared by con
- Sharma, Shilpa,Bedi, Monica,Varshney,Varshney
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- 1-(1-Arylethylidene)thiosemicarbazide derivatives: A new class of tyrosinase inhibitors
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A series of 1-(1-arylethylidene)thiosemicarbazide compounds and their analogues were synthesized and characterized by 1H NMR, MS. Their tyrosinase inhibitory activities were investigated by an assay based on the catalyzing ability of tyrosinase
- Liu, Jinbing,Yi, Wei,Wan, Yiqian,Ma, Lin,Song, Huacan
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p. 1096 - 1102
(2008/09/18)
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- M-STAGE KINESIN INHIBITOR
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A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, -C(=W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents -C(=Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
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Page/Page column 73
(2010/11/08)
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- THIADIAZOLINE DERIVATIVE
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(wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents -C(-W)R6 or the like; R3 represents a hydrogen atom, -C(=WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
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