DESIGN, SYNTHESIS AND EVALUATION OF 6-SUBSTITUTED-4-HYDROXY-1-(2- SUBSTITUTEDACETYL)-3-NITROQUINOLIN-2(1H)-ONEs FOR ANTICANCER ACTIVITY (Record no. 11262)

000 -LEADER
fixed length control field a
003 - CONTROL NUMBER IDENTIFIER
control field OSt
005 - DATE AND TIME OF LATEST TRANSACTION
control field 20200214114505.0
008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION
fixed length control field 200214b xxu||||| |||| 00| 0 eng d
040 ## - CATALOGING SOURCE
Original cataloging agency AIKTC-KRRC
Transcribing agency AIKTC-KRRC
100 ## - MAIN ENTRY--PERSONAL NAME
9 (RLIN) 12268
Author Bhatt, S. S.
245 ## - TITLE STATEMENT
Title DESIGN, SYNTHESIS AND EVALUATION OF 6-SUBSTITUTED-4-HYDROXY-1-(2- SUBSTITUTEDACETYL)-3-NITROQUINOLIN-2(1H)-ONEs FOR ANTICANCER ACTIVITY
250 ## - EDITION STATEMENT
Volume, Issue number Vol.56(12), Dec
260 ## - PUBLICATION, DISTRIBUTION, ETC.
Place of publication, distribution, etc. Mumbai
Name of publisher, distributor, etc. Indian Drug Manufacture's Association - IDMA
Year 2019
300 ## - PHYSICAL DESCRIPTION
Pagination 20-27p.
520 ## - SUMMARY, ETC.
Summary, etc. The present work deals with the synthesis of a series of 6-substituted-4-hydroxy-1-(2-substitued alicyclicaminoacetyl)-3-nitroquinolin-2(1H)-one {IVa-d (1-3)} derivatives and evaluation of their in vitro anticancer activity. Docking study was carried out using EGFR-tyrosine kinase binding site (PDB ID: 1m17) and revealed encouraging results. The sequence of reactions consists of the initial synthesis of 6-substituted 4-hydroxyquinolin-2(1H)-ones (Ia-d), which were further subjected to nitration reaction to give 6- substituted-4-hydroxy-3-nitroquinolin-2(1H)-one (IIa-d). Condensation of compounds (IIa-d) with chloroacetyl chloride resulted in 6-substituted-1-(2-chloroacetyl)-4-hydroxy-3-nitroquinolin-2(1H)-one(IIIa-d), which was subjected to substitution reaction using various secondary amines to yield the title compounds {IVa-d (1-3)}. All the synthesized compounds were characterized by IR, NMR and mass spectral data.All the derivatives were tested for their in vitro anticancer activity using KB (oral cancer) cell lines. Among the synthesized compounds, compound (IVc-2) was found to be the most cytotoxic as compared to the other synthesized derivatives, with IC50 values of 0.2406μM/mL against KB cell line.
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) 12270
Co-Author MaleDesai, S. N.
773 0# - HOST ITEM ENTRY
Title Indian drugs
Place, publisher, and date of publication Mumbai Indian Drug Manufactures Association
856 ## - ELECTRONIC LOCATION AND ACCESS
URL http://www.indiandrugsonline.org/issuesarticle-details?id=MTAwMQ==
Link text Click here
942 ## - ADDED ENTRY ELEMENTS (KOHA)
Source of classification or shelving scheme
Koha item type Articles Abstract Database
Holdings
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 2020-02-14 2020972 2020-02-14 2020-02-14 Articles Abstract Database
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