Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship. 2011

Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.

Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that 2-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.

UI MeSH Term Description Entries
D008297 Male Males
D009369 Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms. Benign Neoplasm,Cancer,Malignant Neoplasm,Tumor,Tumors,Benign Neoplasms,Malignancy,Malignant Neoplasms,Neoplasia,Neoplasm,Neoplasms, Benign,Cancers,Malignancies,Neoplasias,Neoplasm, Benign,Neoplasm, Malignant,Neoplasms, Malignant
D011725 Pyridines Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
D004250 DNA Topoisomerases, Type II DNA TOPOISOMERASES that catalyze ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. These enzymes bring about relaxation of the supercoiled DNA and resolution of a knotted circular DNA duplex. DNA Topoisomerase (ATP-Hydrolysing),DNA Topoisomerase II,DNA Topoisomerase II alpha,DNA Topoisomerase II beta,DNA Type 2 Topoisomerase,TOP2A Protein,TOP2B Protein,Topoisomerase II,Topoisomerase II alpha,Topoisomerase II beta,Type II DNA Topoisomerase,alpha, Topoisomerase II,beta, Topoisomerase II
D004264 DNA Topoisomerases, Type I DNA TOPOISOMERASES that catalyze ATP-independent breakage of one of the two strands of DNA, passage of the unbroken strand through the break, and rejoining of the broken strand. DNA Topoisomerases, Type I enzymes reduce the topological stress in the DNA structure by relaxing the superhelical turns and knotted rings in the DNA helix. DNA Nicking-Closing Protein,DNA Relaxing Enzyme,DNA Relaxing Protein,DNA Topoisomerase,DNA Topoisomerase I,DNA Topoisomerase III,DNA Topoisomerase III alpha,DNA Topoisomerase III beta,DNA Untwisting Enzyme,DNA Untwisting Protein,TOP3 Topoisomerase,TOP3alpha,TOPO IIIalpha,Topo III,Topoisomerase III,Topoisomerase III beta,Topoisomerase IIIalpha,Topoisomerase IIIbeta,DNA Nicking-Closing Proteins,DNA Relaxing Enzymes,DNA Type 1 Topoisomerase,DNA Untwisting Enzymes,DNA Untwisting Proteins,Topoisomerase I,Type I DNA Topoisomerase,III beta, Topoisomerase,III, DNA Topoisomerase,III, Topo,III, Topoisomerase,IIIalpha, TOPO,IIIalpha, Topoisomerase,IIIbeta, Topoisomerase,Topoisomerase III, DNA,Topoisomerase, TOP3,beta, Topoisomerase III
D004268 DNA-Binding Proteins Proteins which bind to DNA. The family includes proteins which bind to both double- and single-stranded DNA and also includes specific DNA binding proteins in serum which can be used as markers for malignant diseases. DNA Helix Destabilizing Proteins,DNA-Binding Protein,Single-Stranded DNA Binding Proteins,DNA Binding Protein,DNA Single-Stranded Binding Protein,SS DNA BP,Single-Stranded DNA-Binding Protein,Binding Protein, DNA,DNA Binding Proteins,DNA Single Stranded Binding Protein,DNA-Binding Protein, Single-Stranded,Protein, DNA-Binding,Single Stranded DNA Binding Protein,Single Stranded DNA Binding Proteins
D004354 Drug Screening Assays, Antitumor Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals. Anticancer Drug Sensitivity Tests,Antitumor Drug Screens,Cancer Drug Tests,Drug Screening Tests, Tumor-Specific,Dye Exclusion Assays, Antitumor,Anti-Cancer Drug Screens,Antitumor Drug Screening Assays,Tumor-Specific Drug Screening Tests,Anti Cancer Drug Screens,Anti-Cancer Drug Screen,Antitumor Drug Screen,Cancer Drug Test,Drug Screen, Anti-Cancer,Drug Screen, Antitumor,Drug Screening Tests, Tumor Specific,Drug Screens, Anti-Cancer,Drug Screens, Antitumor,Drug Test, Cancer,Drug Tests, Cancer,Screen, Anti-Cancer Drug,Screen, Antitumor Drug,Screens, Anti-Cancer Drug,Screens, Antitumor Drug,Test, Cancer Drug,Tests, Cancer Drug,Tumor Specific Drug Screening Tests
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000951 Antigens, Neoplasm Proteins, glycoprotein, or lipoprotein moieties on surfaces of tumor cells that are usually identified by monoclonal antibodies. Many of these are of either embryonic or viral origin. Neoplasm Antigens,Tumor Antigen,Tumor Antigens,Antigen, Tumor,Antigens, Tumor

Related Publications

Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
January 2015, Bioorganic & medicinal chemistry,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
July 2015, Bioorganic & medicinal chemistry,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
May 2013, Bioorganic & medicinal chemistry letters,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
February 2007, Bioorganic & medicinal chemistry,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
April 2004, Bioorganic & medicinal chemistry letters,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
April 2016, Bioorganic & medicinal chemistry,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
April 2005, Bioorganic & medicinal chemistry letters,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
January 2007, Bioorganic & medicinal chemistry,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
February 2006, Bioorganic & medicinal chemistry,
Uttam Thapa, and Pritam Thapa, and Radha Karki, and Minho Yun, and Jae Hun Choi, and Yurngdong Jahng, and Eunyoung Lee, and Kyung-Hwa Jeon, and Younghwa Na, and Eun-Mi Ha, and Won-Jea Cho, and Youngjoo Kwon, and Eung-Seok Lee
March 1995, Journal of medicinal chemistry,
Copied contents to your clipboard!