title: Synthesis, in vitro anticancer and antimycobacterial evaluation of new 5-(2,5-dimethoxyphenyl)-1,3,4-thiadiazole-2-amino derivatives.
abstract: A series of 2,5-disubstituted-1,3,4-thiadiazole derivatives 5a-5l, 7a-7e and 9 have been synthesised and screened for in vitro antimycobacterial activity against Mycobacterium smegmatis MC-155. In addition these compounds have also been screened for cytotoxic activity against cancer cell lines HT-29, MDA-MB-231 by MTT colorimetric assay. The compounds are well characterized by spectral analysis viz. (1)H NMR, (13)C NMR, FT-IR, mass and HRMS. Screening results indicate that compounds 5g, 7a possess good antitubercular activity with MIC value 65.74 and 40.86, respectively, compounds 5g, 7a, 7b, 7d, 7e and 9 displayed promising cytotoxic activity against the cell lines tested. 5g and 7a stand out to be potent antimycobacterial and anticancer agents among the tested series. Further the title compounds were also tested on human normal cells HEK293T and are found to be safer with lesser cytotoxicity. It is interesting to observe that compound 5g has come out to be safer, potent anticancer and antimycobacterial agent.
authors.affiliation: Centre for Chemical Sciences and Technology, IST, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad 500085, T.S., India.
authors.forename: Naveen
authors.initials: N
authors.lastname: Polkam
authors.affiliation: Centre for Chemical Sciences and Technology, IST, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad 500085, T.S., India.
authors.forename: Parsharamulu
authors.initials: P
authors.lastname: Rayam
authors.affiliation: Centre for Chemical Sciences and Technology, IST, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad 500085, T.S., India. Electronic address: jayashreeanireddy@gmail.com.
authors.forename: Jaya Shree
authors.initials: JS
authors.lastname: Anireddy
authors.affiliation: Department of Medicinal Chemistry, GVK Biosciences Pvt. Ltd, IDA, Nacharam, Hyderabad 500076, T.S., India.
authors.forename: Satyanarayana
authors.initials: S
authors.lastname: Yennam
authors.affiliation: Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar 500078, T.S., India.
authors.forename: Hasitha Shilpa
authors.initials: HS
authors.lastname: Anantaraju
authors.affiliation: Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar 500078, T.S., India.
authors.forename: Sriram
authors.initials: S
authors.lastname: Dharmarajan
authors.affiliation: Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad Campus, Jawahar Nagar 500078, T.S., India.
authors.forename: Yogeeswari
authors.initials: Y
authors.lastname: Perumal
authors.affiliation: Center for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, T.S., India.
authors.forename: Sudha Sravanti
authors.initials: SS
authors.lastname: Kotapalli
authors.affiliation: Center for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, T.S., India.
authors.forename: Ramesh
authors.initials: R
authors.lastname: Ummanni
authors.affiliation: Laboratory of X-ray Crystallography, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, T.S., India.
authors.forename: Sridhar
authors.initials: S
authors.lastname: Balasubramanian
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D057809:HEK293 Cells; D019073:HT29 Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D020102:Mycobacterium smegmatis / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents
keywords: 2,5-Disubstitued-1,3,4-thiadiazole; Anti-mycobacterial activity; Cytotoxic activity; In vitro studies; MTT colorimetric assay