000			a
999			_c8995 _d8995
003			OSt
005			20190514114343.0
008			190514b xxu||||| |||| 00| 0 eng d
040			_aAIKTC-KRRC _cAIKTC-KRRC
100			_98500 _aBahmani, Y.
245			_aSynthesis, Cytotoxicity Assessment and Molecular Docking of N-(5-(substituted-benzylthio)-1,3,4-thiadiazole-2-yl)-2-p-fluorophenylacetamide Derivatives as Tyrosine Kinase Inhibitors
250			_aVol. 81(1), Jan-Feb
260			_aMumbai _bIndian Journal of Pharmaceutical Science _c2019
300			_a63-70p.
520			_aCompounds containing 1,3,4-thiadiazole nucleus appear to be potential tyrosine kinase inhibitors. Previous reports showed that some 1,3,4-thiadiazole derivatives were designed as probable tyrosine kinase inhibitors. Thiol derivative (2) was obtained from the reaction of 5-amino-1,3,4-thiadiazole-2-thiol with 4-fluorophenylacetic acid, ethyldimethyaminopropylcarbodiimide and hydroxybenzotriazole. Subsequent reaction of the obtained thiol derivative with diverse benzyl chlorides afforded the final compounds 3a-3l in a click reaction surprisingly. Derivatives with electron withdrawing moieties (F, Cl) exerted higher yield compared to methoxylated derivatives as electron donating group. Besides, docking studies using ArgusLab 4.0 was done for exploring the probable binding mode and interactions. Investigation of cytotoxicity of target compounds (3a-3l) by MTT assay revealed that these derivatives are more active against the breast cancer cell line MCF-7 and most of these were found to be more effective than imatinib as reference drug. Chlorine containing derivatives at ortho and meta positions were the most cytotoxic in these series
650		0	_94639 _aPHARMACEUTICS
700			_98501 _aBahrami, T.
700			_98502 _aAliabadi, A.
773	0		_x0250-474X _tIndian journal of pharmaceutical sciences _dNew Delhi Indian Pharmaceutical Association
856			_uhttp://www.ijpsonline.com/articles/synthesis-cytotoxicity-assessment-and-molecular-docking-of-n5substitutedbenzylthio134thiadiazole2yl2pfluorophenylacetami.pdf _yClick here
942			_2ddc _cAR