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Title: An efficient protocol for the synthesis of β-substituted ethyl dithiocarbamates: A novel class of anti-cancer agents
Authors: Chaturvedi, Devdutt
Zaidi, Sadaf
Chaturvedi, Amit K
Vaid, Shagun
Saxena, Ajit K
Keywords: Amines;α,β-unsaturated activated olefins;Carbon disulfide;Triton-B;Dithiocarbamates;Anticancer activity
Issue Date: Aug-2016
Publisher: NISCAIR-CSIR, India
Abstract: A novel one-pot method for the synthesis of β-substituted alkyl dithiocarbamates has been developed through the Michael addition reaction of dithiocarbamate anion to α,β-unsaturated activated olefins employing catalytic amount of benzyl trimethyl ammonium hydroxide (Triton-B). The reaction conditions are mild with extremely simple work-up procedures than the reported methods, and afford high yields (82-98%) of the desired products. All the synthesized compounds (1-16) have been evaluated for in vitro anti-cancer activity using various kinds of cancer cell lines such as lung, colon, cervical, neuroblastoma, liver and ovary employing different kinds of standard anticancer drugs such as 5-fluorouracil, mitomycin C, paclitaxel, aldriamycin, etc. using stock solution (2 × 10−2 M) prepared in DMSO and further dilution has been carried out with medium. In vitro cytotoxicity against human cancer cell lines is determined using sulphorhodamine-B assay. Out of the series of compounds evaluated, most of these compounds such as compounds 2, 3, 4, 5, 9, 10, 11, 12, 13, 14, 15, 16 display more than 50% growth inhibition at 1 × 10−5 M concentration.
Page(s): 1019-1025
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.55B(08) [August 2016]

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