ChemInform Abstract: 5‐Chloro‐3‐(phenylsulfonyl)indole‐2‐carboxamide: A Novel, Non‐ Nucleoside Inhibitor of HIV‐1 Reverse Transcriptase.

Abstract

WILLIAMS, T. M.; CICCARONE, T. M.; MACTOUGH, S. C.; ROONEY, C. S.; BALANI, S. K.; CONDRA, J. H.; EMINI, E. A.; GOLDMAN, M. E.; GREENLEE, W. J.; KAUFFMAN, L. R.; O'BRIEN, J. A.; SARDANA, V. V.; SCHLEIF, W. A.; THEOHARIDES, A. D.; ANDERSON, P. S.; J. Med.

N-Pyrrylarylsulfones with High Therapeutic Potential

“…The highly potent anti-HIV-1 activity displayed by Merck carboxamide L-737,126 ( 78 ) [ 74 , 75 , 76 ] (HIV-1 WT IIIB EC 50 = 1 nM; HIV-1 RT IC 50 = 25 nM) prompted the design of new indolylarylsulfone (IAS) analogs. Due to the lack of SAR information, the design of first IAS derivatives was based on PASs’ structural features.…”

Electrochemical synthesis of the new substituted phenylpiperazines

“…Some of diphenylsulfones have been shown to inhibit HIV-1 reverse transcriptase and represent an emerging class of substances able to address toxicity and resistance problems of nucleoside inhibitors [3,4]. They are useful in the practice of medicinal chemistry because the sulfone functional group is found in numerous drugs [5].…”

Synthesis of 3-Sulfenyl- and 3-Selenylindoles by the Pd/Cu-Catalyzed Coupling of N,N-Dialkyl-2-iodoanilines and Terminal Alkynes, Followed by n-Bu4NI-Induced Electrophilic Cyclization

“…For instance, MK-886 is an inhibitor of 5-lipoxygenase and can augment the antitumor activity of celecoxib in human colorectal cancer 7. L-737,126 is known to exhibit potent anti-HIV properties,8 and the 3-(arylsulfenyl)indole 1 is not only an inhibitor of tubulin polymerization, but also capable of inhibiting human breast cancer cell growth 9…”