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 |