Organoboronic acids/esters as effective drug and prodrug candidates in cancer treatments: challenge and hope.

Boronic acids/esters have recently emerged in the field of medicinal and pharmaceutical research due to their exceptional oxophilicity, low toxicity, and unique structure. They are known as potent enzyme inhibitors, cancer therapy capture agents, and can mimic certain types of antibodies to fight infections. They have been designed and developed into drugs, and this approach has emerged in the last 20 years. Five boronic acid drugs have been approved by the FDA and Health Canada, two of which are used to treat cancer, specifically multiple myeloma. The purpose of this review is to investigate boronic acid/ester derivatives as potential pharmaceutical agents as well as the mechanism of action. It will concentrate on six types of cancer: multiple myeloma, prostate cancer, breast cancer, lung cancer, cervical cancer, and colon cancer. Some newly developed boron-containing compounds have already demonstrated highly promising activities, but further investigation is required before final conclusions can be drawn.

Palladium-catalyzed highly regioselective mono and double Sonogashira cross-coupling reactions of 5-substituted-1,2,3-triiodobenzene under ambient conditions.

An efficient synthesis of 2,3-diiodinated diphenylacetylene and iodinated meta-terphenylacetylene derivatives through highly regioselective mono and double Sonogashira cross-coupling reactions of 5-substituted-1,2,3-triiodobenzene is reported. Significantly, the regioselectivity of coupling reactions is exclusively performed at the terminal C-I bonds, the less sterically hindered and the most regioactive positions. The highest isolated yields were achieved from reactions of electron-poor/neutral 1,2,3-triiodoarene and electron-rich arylacetylene derivatives. The use of 2.0 equiv. of arylacetylenes in one-pot fashion afforded the iodinated meta-terphenylacetylenes in excellent site selectivity and in good isolated yields. Different functional groups were found to be suitable under optimized conditions. This report discloses the first method to synthesize hitherto unknown 2,3-diiodinated diphenylacetylenes and iodinated meta-terphenylacetylenes that is facile, highly regioselective, general in scope and produces remarkable building blocks for other chemical transformations.