Ravi Kumar Bommera1, Shashikala Kethireddy2, Rajeshwar Reddy Govindapur3, Laxminarayana Eppakayala4. 1. Sreenidhi Institute of Science and Technology (Autonomous), Yamnampet, Ghatkesar, Hyderabad, Telangana, India. 2. Geethanjali College of Engineering and Technology, (Autonomous), Cheeryal, Keesara, Hyderabad, Telangana, India. 3. University of North Carolina Wilmington, Wilmington, NC, 28409, USA. 4. Sreenidhi Institute of Science and Technology (Autonomous), Yamnampet, Ghatkesar, Hyderabad, Telangana, India. elxnkits@yahoo.co.in.
Abstract
BACKGROUND: 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β3-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. But its application is limited, as it has side effects like low bioavailability and high toxicity. Molecular docking is an exemplary tool, helps in identifying target and designing a drug containing high bio-availability and minimum toxicity. RESULTS: A set of 1,2,4-oxadiazole linked 5-fluoruracil derivatives (7a-j) were synthesized and their structures were confirmed by 1HNMR, 13CNMR and Mass spectral analysis. Further, these compounds were investigated for their anticancer activity towards a panel of four human cancer cell lines such as (MCF-7, MDA MB-231), lung cancer (A549) and prostate cancer (DU-145) by using MTT method. Among them, compounds 7a, 7b, 7c, 7d and 7i demonstrated more promising anticancer activity than standard. CONCLUSION: Synthesized derivatives (7a-j) of 1,2,4-oxadiazole linked 5-fluorouracil and investigated for their anticancer activity towards a panel of four human cancer cell lines.
BACKGROUND:1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against humancancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β3-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. But its application is limited, as it has side effects like low bioavailability and high toxicity. Molecular docking is an exemplary tool, helps in identifying target and designing a drug containing high bio-availability and minimum toxicity. RESULTS: A set of 1,2,4-oxadiazole linked 5-fluoruracil derivatives (7a-j) were synthesized and their structures were confirmed by 1HNMR, 13CNMR and Mass spectral analysis. Further, these compounds were investigated for their anticancer activity towards a panel of four humancancer cell lines such as (MCF-7, MDA MB-231), lung cancer (A549) and prostate cancer (DU-145) by using MTT method. Among them, compounds 7a, 7b, 7c, 7d and 7i demonstrated more promising anticancer activity than standard. CONCLUSION: Synthesized derivatives (7a-j) of 1,2,4-oxadiazole linked 5-fluorouracil and investigated for their anticancer activity towards a panel of four humancancer cell lines.
Entities:
Keywords:
5-Fluorouracil; Ataluren; Oxadiazole and anticancer activity; Pyrimidine
Authors: C HEIDELBERGER; N K CHAUDHURI; P DANNEBERG; D MOOREN; L GRIESBACH; R DUSCHINSKY; R J SCHNITZER; E PLEVEN; J SCHEINER Journal: Nature Date: 1957-03-30 Impact factor: 49.962
Authors: Lucía Cordeu; Elena Cubedo; Eva Bandrés; Amaia Rebollo; Xabi Sáenz; Hector Chozas; Ma Victoria Domínguez; Mikel Echeverría; Beatriz Mendivil; Carmen Sanmartin; Juan Antonio Palop; María Font; Jesús García-Foncillas Journal: Bioorg Med Chem Date: 2006-12-12 Impact factor: 3.641
Authors: Emily E Dando; Geoffrey F S Lim; Scott J M Lim; ChangHyun Kim; Melissa Pugliano-Mauro Journal: Dermatol Surg Date: 2020-01 Impact factor: 3.398
Authors: P Noordhuis; U Holwerda; C L Van der Wilt; C J Van Groeningen; K Smid; S Meijer; H M Pinedo; G J Peters Journal: Ann Oncol Date: 2004-07 Impact factor: 32.976