Synthesis, anti-proliferative and genotoxicity studies of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2 H-indol-2-ones and 6-chloro-5-(2-chloroethyl)-3-(alkyl/ary-2-ylidene)indolin-2-ones

Gangadhar Y. Meti; Atulkumar A. Kamble; Ravindra R. Kamble; Shilpa M. Somagond; H. C. Devarajegowda; Sandhya Kumari; Guruprasad Kalthur; Satish K. Adiga

doi:10.1016/j.ejmech.2016.05.028

Synthesis, anti-proliferative and genotoxicity studies of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2 H-indol-2-ones and 6-chloro-5-(2-chloroethyl)-3-(alkyl/ary-2-ylidene)indolin-2-ones

Gangadhar Y. Meti
, Atulkumar A. Kamble
, Ravindra R. Kamble^*
, Shilpa M. Somagond
, H. C. Devarajegowda
, Sandhya Kumari
, Guruprasad Kalthur
, Satish K. Adiga

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

5 Citations (Scopus)

Abstract

A series of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2H-indol-2-ones (3a-h) and 6-chloro-5-(2-chloroethyl)-3-(alkyl/aryl-2-ylidene)indolin-2-ones (5i-x) were synthesized. Compounds 3a-e, 5i-l and 5q-r were selected by NIH, USA for in vitro anti-proliferative screening. Based on the impressive growth inhibitory (GI %) effect by the compounds 3a-b and 3e which showed growth inhibition in the range 1.22-76.30%, 2.85-76.03% and 10.98-82.05% respectively at 10^ĝ'5 concentration, these compounds were further analyzed for anti-proliferative activity at 5 dose concentration and genotoxicity.

Original language	English
Pages (from-to)	221-231
Number of pages	11
Journal	European Journal of Medicinal Chemistry
Volume	121
DOIs	https://doi.org/10.1016/j.ejmech.2016.05.028
Publication status	Published - 04-10-2016

All Science Journal Classification (ASJC) codes

Pharmacology
Drug Discovery
Organic Chemistry

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10.1016/j.ejmech.2016.05.028

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Meti, G. Y., Kamble, A. A., Kamble, R. R., Somagond, S. M., Devarajegowda, H. C., Kumari, S., Kalthur, G., & Adiga, S. K. (2016). Synthesis, anti-proliferative and genotoxicity studies of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2 H-indol-2-ones and 6-chloro-5-(2-chloroethyl)-3-(alkyl/ary-2-ylidene)indolin-2-ones. European Journal of Medicinal Chemistry, 121, 221-231. https://doi.org/10.1016/j.ejmech.2016.05.028

@article{1cb9ee443c984ca39563db0994bdcd63,

title = "Synthesis, anti-proliferative and genotoxicity studies of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2 H-indol-2-ones and 6-chloro-5-(2-chloroethyl)-3-(alkyl/ary-2-ylidene)indolin-2-ones",

abstract = "A series of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2H-indol-2-ones (3a-h) and 6-chloro-5-(2-chloroethyl)-3-(alkyl/aryl-2-ylidene)indolin-2-ones (5i-x) were synthesized. Compounds 3a-e, 5i-l and 5q-r were selected by NIH, USA for in vitro anti-proliferative screening. Based on the impressive growth inhibitory (GI \%) effect by the compounds 3a-b and 3e which showed growth inhibition in the range 1.22-76.30\%, 2.85-76.03\% and 10.98-82.05\% respectively at 10ĝ'5 concentration, these compounds were further analyzed for anti-proliferative activity at 5 dose concentration and genotoxicity.",

author = "Meti, \{Gangadhar Y.\} and Kamble, \{Atulkumar A.\} and Kamble, \{Ravindra R.\} and Somagond, \{Shilpa M.\} and Devarajegowda, \{H. C.\} and Sandhya Kumari and Guruprasad Kalthur and Adiga, \{Satish K.\}",

note = "Publisher Copyright: {\textcopyright} 2016 Elsevier Masson SAS.",

year = "2016",

month = oct,

day = "4",

doi = "10.1016/j.ejmech.2016.05.028",

language = "English",

volume = "121",

pages = "221--231",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

Meti, GY, Kamble, AA, Kamble, RR, Somagond, SM, Devarajegowda, HC, Kumari, S, Kalthur, G & Adiga, SK 2016, 'Synthesis, anti-proliferative and genotoxicity studies of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2 H-indol-2-ones and 6-chloro-5-(2-chloroethyl)-3-(alkyl/ary-2-ylidene)indolin-2-ones', European Journal of Medicinal Chemistry, vol. 121, pp. 221-231. https://doi.org/10.1016/j.ejmech.2016.05.028

Synthesis, anti-proliferative and genotoxicity studies of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2 H-indol-2-ones and 6-chloro-5-(2-chloroethyl)-3-(alkyl/ary-2-ylidene)indolin-2-ones. / Meti, Gangadhar Y.; Kamble, Atulkumar A.; Kamble, Ravindra R. et al.
In: European Journal of Medicinal Chemistry, Vol. 121, 04.10.2016, p. 221-231.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - Synthesis, anti-proliferative and genotoxicity studies of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2 H-indol-2-ones and 6-chloro-5-(2-chloroethyl)-3-(alkyl/ary-2-ylidene)indolin-2-ones

AU - Meti, Gangadhar Y.

AU - Kamble, Atulkumar A.

AU - Kamble, Ravindra R.

AU - Somagond, Shilpa M.

AU - Devarajegowda, H. C.

AU - Kumari, Sandhya

AU - Kalthur, Guruprasad

AU - Adiga, Satish K.

PY - 2016/10/4

Y1 - 2016/10/4

N2 - A series of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2H-indol-2-ones (3a-h) and 6-chloro-5-(2-chloroethyl)-3-(alkyl/aryl-2-ylidene)indolin-2-ones (5i-x) were synthesized. Compounds 3a-e, 5i-l and 5q-r were selected by NIH, USA for in vitro anti-proliferative screening. Based on the impressive growth inhibitory (GI %) effect by the compounds 3a-b and 3e which showed growth inhibition in the range 1.22-76.30%, 2.85-76.03% and 10.98-82.05% respectively at 10ĝ'5 concentration, these compounds were further analyzed for anti-proliferative activity at 5 dose concentration and genotoxicity.

AB - A series of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2H-indol-2-ones (3a-h) and 6-chloro-5-(2-chloroethyl)-3-(alkyl/aryl-2-ylidene)indolin-2-ones (5i-x) were synthesized. Compounds 3a-e, 5i-l and 5q-r were selected by NIH, USA for in vitro anti-proliferative screening. Based on the impressive growth inhibitory (GI %) effect by the compounds 3a-b and 3e which showed growth inhibition in the range 1.22-76.30%, 2.85-76.03% and 10.98-82.05% respectively at 10ĝ'5 concentration, these compounds were further analyzed for anti-proliferative activity at 5 dose concentration and genotoxicity.

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UR - https://www.scopus.com/pages/publications/84971330880#tab=citedBy

U2 - 10.1016/j.ejmech.2016.05.028

DO - 10.1016/j.ejmech.2016.05.028

M3 - Article

C2 - 27240276

AN - SCOPUS:84971330880

SN - 0223-5234

VL - 121

SP - 221

EP - 231

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Synthesis, anti-proliferative and genotoxicity studies of 6-chloro-5-(2-substituted-ethyl)-1,3-dihydro-2 H-indol-2-ones and 6-chloro-5-(2-chloroethyl)-3-(alkyl/ary-2-ylidene)indolin-2-ones

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