Synthetic Novel Flavanoid derivatives act as Potential Antineoplastic Agent

Asish Bhaumik *¹, B. Ramu², Sk. Basheer³, Prasenjit Das⁴, J.Mastanaiah^5
1,3Department of Pharmaceutical Chemistry, Teja College of Pharmacy, Kodad, Nalgonda-508206, Telangana State, India.
²Department of Biochemistry, MITS College of Pharmacy, Kodad, Nalgonda-508206, Telangana State,  India.
⁴Department of Pharmaceutical Chemistry, Regional Institute of Pharmaceutical Science & Technology, Abhoynagar, Agartala-799005, Tripura, India.
⁵Department of Pharmacology, GATE School of Pharmacy, Kodad, Nalgonda-508206, Telangana, State, India.

A B S T R A C T
Neoplasm or tumour is a mass of tissue formed as a result of abnormal, excessive, uncoordinated, autonomas and purposeless proliferation of cells. The main objective of the present work was the synthesis of 2- (2, 3, 4, & 5 substituted phenyl) 3-hydroxy-4H-Chromen-4-one and evaluation of in-vitro antineoplastic activity. The synthesized compounds were characterized by IR, NMR, and Mass spectroscopy. The in-vitro antineoplastic activities were carried out against Human Prostate cancer cell line DU-145 and Human Leukemia Cancer Cell line MOLT- 4 and SRB assay was used to analyze the cell growth inhibition of the both cancer cell lines. The results had been showed that compound 4A- 4J were possessed an excellent antineoplastic activity (at 25 µg/ml) against both cancer cell lines. 5-Fluro uracil (5-FU, at 15µg/ml ) was used as a standard drug for DU-145 cell line and doxorubicin (at 15µg/ml) was used as a standard drug for MOLT-4 cell. IC₅₀  values of the synthesized compounds were found to be 4A (IC₅₀ of2.2 µg/ml), 4B (IC₅₀ of 2.3 µg/ml), 4C (IC₅₀ of 2.6 µg/ml), 4D (IC₅₀ of 2.8 µg/ml), 4E (IC₅₀ of 3.1 µg/ml), 4F (IC₅₀ of 2.9 µg/ml), 4G (IC₅₀ of 2.3 µg/ml), 4H (IC₅₀ of 3.4 µg/ml), 4I (IC₅₀ of 3.8 µg/ml)  and 4J (IC₅₀ of 2.0 µg/ml) against DU-145 cell line and  4A (IC₅₀ of2.3 µg/ml), 4B (IC₅₀ of 2.4 µg/ml), 4C (IC₅₀ of 2.5 µg/ml), 4D (IC₅₀ of 2.7 µg/ml), 4E (IC₅₀ of 2.9 µg/ml), 4F (IC₅₀ of 3.1 µg/ml), 4G (IC₅₀ of 3.3 µg/ml), 4H (IC₅₀ of 4.3 µg/ml), 4I (IC₅₀ of 3.9 µg/ml)  and 4J (IC₅₀ of 2.2 µg/ml) against MOLT-4 cell line. The IC₅₀ values of standard drugs  5-FU and doxorubicin were found to be 1.88 µg/ml and 1.91 µg/ml.
Keywords: Chromen, Neoplasia, Antineoplastic activity DU-145, MOLT-4, SRB assay,  IC₅₀