Synthesis and Anti-cancer activity of new optically active 1,3,4-thiadiazole derivatives acting as histone deacetylase inhibitors by rational approach.

Atodaria Bhavini ^*, Thakor Vanraj , Hassani Jagruti , Bhayani Fenil,  Noolvi Malleshappa 

Shree dhanvantary College of pharmacy, Kim, Surat, Gujarat, India

ABSTRACT

Histone deacetylase (HDACs) play a key role in homeostasis of protein acetylation in histones and other proteins and in regulating fundamental cellular activities such as transcription. A wide range of tumors are associated with imbalances in protein acetylation levels and transcriptional dysfunctions. Treatment with various HDAC inhibitors can correct these deficiencies and has emerged as a promising new strategy for therapeutic intervention in anticancer disease. 1,3,4-thiadiazoles represents an important heterocyclic system due to their pharmacological activity like anti-bacterial, anti-fungal, anti-epileptic, antiulcer, anti-mycobacterial, anti-inflammatory, anti-cancer. Here, we review and discuss intriguing recent developments in the use of HDAC inhibitors to combat anticancer conditions in cellular and disease models. We discuss the targets and mechanisms underlying these effects of HDAC inhibition and comment on the potential for some HDAC inhibitors to prove clinically effective in the treatment of anticancer activity. New optically active 1,3,4-thiadiazole derivatives containing heterocyclic are synthesized by using simple starting materials like optically active stereo center containing amino acid like L-alanine by protection of the amino group with the help of BOC anhydride to convert amino acid to lead to formation of thiadiazole by Cyclization using simple laboratory conditions and followed by attachment of different heterocycle including benzothiazole to form thiadiazole derivatives.

Keywords: Cancer, chiral, L-alanine, benzothiazole, histone deacetylase.