Synthesis, anti HIV-1 reverse transcriptase and cytotoxic activity of phthalimide derivatives
2
Issued Date
2007
Copyright Date
2007
Resource Type
Language
eng
File Type
application/pdf
No. of Pages/File Size
xv, 87 leaves : ill.
Access Rights
open access
Rights
ผลงานนี้เป็นลิขสิทธิ์ของมหาวิทยาลัยมหิดล ขอสงวนไว้สำหรับเพื่อการศึกษาเท่านั้น ต้องอ้างอิงแหล่งที่มา ห้ามดัดแปลงเนื้อหา และห้ามนำไปใช้เพื่อการค้า
Rights Holder(s)
Mahidol University
Bibliographic Citation
Thesis (M.Sc. (Pharmaceutical Chemistry and Phytochemistry))--Mahidol University, 2007
Suggested Citation
Suratsawadee Piyaviriyakul Synthesis, anti HIV-1 reverse transcriptase and cytotoxic activity of phthalimide derivatives. Thesis (M.Sc. (Pharmaceutical Chemistry and Phytochemistry))--Mahidol University, 2007. Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/96957
Title
Synthesis, anti HIV-1 reverse transcriptase and cytotoxic activity of phthalimide derivatives
Alternative Title(s)
การสังเคราะห์ การทดสอบฤทธิ์ต้านเอนไซม์ HIV-1 reverse transcriptase และความเป็นพิษต่อเซลล์มะเร็งของอนุพันธ์ phthalimide
Author(s)
Advisor(s)
Abstract
The novel phthalimide derivatives were designed and synthesized by modifying of the phthalimide structures based on the three-dimensional quantitative structure-activity relationship (3D QSAR), comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) studies. These derivatives were synthesized using phthalimide and substituted benzyl halide in the presence potassium hydroxide. Six newly synthesized compounds were evaluated for HIV-1 reverse transcriptase inhibitory activity by radioactivity assay at concentration 200 ug/mL using poly(rA).oligo(dT) as template-primer, methyl- [3H]dTTP as substrate and doxorubicin (1.25 mM) as positive control. The synthesized compounds showed low inhibitory activity in the range of 7.9-22.9 % inhibition. Since infection with HIV-1 is associated with an increased risk of developing certain types of cancer, the previously and newly synthesized phthalimide derivatives have been subjected to cytotoxic activity testing using MTT colorimetric method against the cancer cell lines KB and HeLa and normal vero cell line. 1- Phthalimidomethyl-4-tert-butylbenzene, compound 36 demonstrated promising cytotoxic activity that was less toxic to normal cells.
Description
Pharmaceutical Chemistry and Phytochemistry (Mahidol University 2007)
Degree Name
Master of Science
Degree Level
Master's degree
Degree Department
Faculty of Pharmacy
Degree Discipline
Pharmaceutical Chemistry and Phytochemistry
Degree Grantor(s)
Mahidol University