Jawaharlal Nehru Centre for Advanced Scientific Research

Karanam Balasubramanyam

Tapas Kumar Kundu

Venkatesh Swaminathan

Kempegowda Mantelingu

Altaf Mohammad

A Varier Radhika

Kundu Tapas Kumar

Vankatesh Swaminathan

The invention provides the use of certain benzoic acid and benzamide compounds as modulators of enzymes histone acetyltransferases, which are involved in gene expression and cancer and also use of such compounds in the treatment of diseases due to defects in gene regulation predominantly cancer. 

Modulators (inhibitors/activators) of histone acetyltransferases

In this patent we describe the purification of prenylated benzophenones from the fruit rinds ofspecies and its evaluation as an inhibitor for Histone acetyltransferases p300 and PCAF. We have found that prenylated benzophenones are potent HAT inhibitors of p300 (IC-1 &#x3bc;M) and pCAF (IC-15 &#x3bc;M). The inhibitors significantly repress the p300 HAT dependent transcriptional activation from in vitro assembled chromatin template but had no effect on transcription from DNA. These results suggest that the compounds could be specific to HATs. Thus these compounds should be useful as biological switching molecule for evaluating the role of p300 and PCAF in cellular functions and may be useful as new chemical entities for the development of anticancer drugs. 

Polyisoprenylated benzophenones and their isomers as inhibitors of histone acetyltransferases and uses thereof

Disclosed are compounds of the formulae: and method of using the compounds to treat cancer, AIDS, HIV infection, and asthma.

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Karanam Balasubramanyam