Sequential Cytotoxicity: A Theory Examined Using 2, 6 diphenyl Piperidine-4-one scaffold | Chapter 6 | Current Research and Development in Chemistry Vol. 2

The concept of sequential cytotoxicity indicates the successive release of two or more cytotoxic compounds causing grater toxicity to the neoplasm than normal cell. This hypothesis is evaluated by designing a series of compounds of 2, 6 diphenyl piperidine-4-one. Recently for the development of novel cytotoxic and anticancer agents, different series of compounds have been designed that utilizes the 1, 5-diaryl-3-oxo-1, 4-pentadinyel pharmacophore. These compounds interact with cellular thiols of cell and thiols are not part of nucleic acids. Hence these compounds are free from the problem of mutagenicity and carcinogenicity. The series of compounds which either lacking of olefinic bond or one or more olefinic bond are synthesized by Claisen-Schmith reaction. The compounds having one or no any olefinic bonds will be predicted to be less cytotoxic than the compounds having two or three olefinic bonds. The SRB-assay method was used to evaluate cytotoxic property of all the synthesized compounds. The results revealed that the predictions made regarding the viability of the theory of sequential cytotoxicity were fulfilled.

Author(s) Details

Dr. Rahul L. Jadhav
Gourishankar Institute of Pharmaceutical Education and Research, Limb, Satara, Maharashtra, India.

Dr. Chandrakant S. Magdum
K. E. Society’s Rajarambapu College of Pharmacy, Kasegaon, Sangli, Maharashtra, India.

Miss. Manisha V. Patil
Adarsh College of Pharmacy, Vita, Sangli, Maharashtra, India.

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