Design Synthesis and Evaluation of Coumarin and Chromene Analogs for Breast Cancer

Abstract

Cancer has emerged as a deadliest disease, and the different types of cancer such as lung, stomach, breast, and prostate cancer are life-threatening. Breast cancer has surpassed lung cancer in its incidence. The causative factors include family history, age, lifestyle disorders such as obesity, physical inactivity etc., wherein approximately 75% is due to the expression of Estrogen receptor (ER). It is studied that an extragonadal biosynthesis of estrogens promotes tumorigenesis. newlineThe increase in circulation of estrogens is attributed to two specific enzymes, aromatase and steroidal sulfatase. The enzyme aromatase plays a role in conversion of androgens to estrogens, and steroidal sulfatase converts estrogens to Estradiol (E2). The hormone estrogen exists in three forms, Estrone (E1), Estradiol (E2) and Estriol (E3). Of the three forms, E2 stimulates cancer growth. E1 is in active form as E1S (Estrone sulphate), which is further converted to E2 using 17-and#946; Hydroxy steroid dehydrogenase. E2 gets activated and leads to mitotic cancer growth. In the development of lead candidates preventing the formation of E2, STS target is preferred over aromatase. The wide distribution and higher expression of STS make it an attractive target newline