Synthesis, Cytotoxicity Assessment and Molecular Docking of N-(5-(substituted-benzylthio)-1,3,4-thiadiazole-2-yl)-2-p-fluorophenylacetamide Derivatives as Tyrosine Kinase Inhibitors (Record no. 8995)

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control field OSt
005 - DATE AND TIME OF LATEST TRANSACTION
control field 20190514114343.0
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040 ## - CATALOGING SOURCE
Original cataloging agency AIKTC-KRRC
Transcribing agency AIKTC-KRRC
100 ## - MAIN ENTRY--PERSONAL NAME
9 (RLIN) 8500
Author Bahmani, Y.
245 ## - TITLE STATEMENT
Title Synthesis, 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 ## - EDITION STATEMENT
Volume, Issue number Vol. 81(1), Jan-Feb
260 ## - PUBLICATION, DISTRIBUTION, ETC.
Place of publication, distribution, etc. Mumbai
Name of publisher, distributor, etc. Indian Journal of Pharmaceutical Science
Year 2019
300 ## - PHYSICAL DESCRIPTION
Pagination 63-70p.
520 ## - SUMMARY, ETC.
Summary, etc. Compounds 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 - SUBJECT ADDED ENTRY--TOPICAL TERM
9 (RLIN) 4639
Topical term or geographic name entry element PHARMACEUTICS
700 ## - ADDED ENTRY--PERSONAL NAME
9 (RLIN) 8501
Co-Author Bahrami, T.
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9 (RLIN) 8502
Co-Author Aliabadi, A.
773 0# - HOST ITEM ENTRY
International Standard Serial Number 0250-474X
Title Indian journal of pharmaceutical sciences
Place, publisher, and date of publication New Delhi Indian Pharmaceutical Association
856 ## - ELECTRONIC LOCATION AND ACCESS
URL http://www.ijpsonline.com/articles/synthesis-cytotoxicity-assessment-and-molecular-docking-of-n5substitutedbenzylthio134thiadiazole2yl2pfluorophenylacetami.pdf
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Source of classification or shelving scheme
Koha item type Articles Abstract Database
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Withdrawn status Lost status Source of classification or shelving scheme Damaged status Not for loan Permanent Location Current Location Shelving location Date acquired Barcode Date last seen Price effective from Koha item type
          School of Pharmacy School of Pharmacy Archieval Section 2019-05-14 2018499 2019-06-19 2019-05-14 Articles Abstract Database
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