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Hwan-Mook Kim

Publications and source records attributed to Hwan-Mook Kim.

24 records · Page 2Linked to original sources
PubMed2002

Preliminary structure-antiangiogenic activity relationships of 4-senecioyloxymethyl-6,7-dimethoxycoumarin.

Through a systematic modification of the novel angiogenesis inhibitor 4-senecioyloxymethyl-6,7-dimethoxycoumarin (1) we found that a 6,7-dimethoxy moiety is important for bioactivity of 1. Replacement of the lactone functionality in coumarin 1 by an amide decreased its activity. By substitution of the senecioyl chain with various cinnamoyl groups we discovered 6d, bearing a 4-methoxycinnamoyl instead of senecioyl side chain, with inhibitory activity in HUVEC tube formation assay enhanced by one order of magnitude compared to 1. We have also synthesized compound 12, an analogue of 6d, with equipotency and improved water solubility.

Angiogenesis Inhibitors↗
PubMed2002

Synthesis and anti-tumor activity of novel combretastatins: combretocyclopentenones and related analogues.

A series of 2-(3,4,5-trimethoxyphenyl)-3-arylcyclopent-2-ene-1-ones (8a-8e) and their related analogues, including pentenone 9a, pentenol 10a, pentene 12a, and furane 15, were synthesized and evaluated for cytotoxicity against murine and human tumor cell lines. Compounds 8a-c, 8e and 9a showed strong cytotoxicity with IC(50) values in the range of 8-34ng/mL. Compound 8e exhibited significant anti-tumor activity in BDF1 mice bearing Lewis lung carcinoma cells with an inhibition ratio of 59%.

Animals↗
PubMed2002

Synthesis and cytotoxicity of some rigid derivatives of methyl 2,5-dihydroxycinnamate.

Eight rigid compounds designed as esterase-stable analogues of methyl 2,5-dihydroxycinnamate (1) were synthesized. These derivatives include 2-(2',5'-dihydroxybenzylidene)cyclopentenone (3a), 2-(2',5'-dihydroxybenzylidene)cyclohexanone (3b), 2,6-bis(2',5'-dihydroxybenzylidene)cyclohexanone (4b), 2,6-bis(2',5'-dihydroxybenzylidene)cyclopentenone (4a), (E)-3-(2',5'-dihydroxybenzylidene)pyrrolidin-2-one (5), (E)-5-(2',5'-dihydroxybenzylidene)-1,2-isothiazolidine-1,1-dioxide (6), 4-(2',5'-dihydroxyphenyl)-5H-furan-2-one (7), and 3-(2',5'-dihydroxyphenyl)cyclopent-2-ene-1-one (8). Among the eight compounds, the furanone 7 and cyclopentenone 8 showed the most potent cytotoxicity with IC50 values of 0.39-0.98 microg/mL. Compound 8 was further brominated, phenylated and methylated at the alpha position to give three corresponding analogues, including 2-bromo-3-(2',5'-dihydroxyphenyl)cyclopent-2-ene-1-one (24), 3-(2',5'-dihydroxyphenyl)-2-phenylcyclopent-2-ene-1-one (27), and 3-(2',5'-dihydroxyphenyl)-2-methylcyclopent-2-ene-1-one (28). Among the three, the most enhanced activity was observed with the phenylated compound 27.

Animals↗
PubMed2002

Synthesis, cytotoxicity and antitumor activity of 2,3-diarylcyclopent-2-ene-1-ones.

Two series of 2,3-diarylcyclopent-2-ene-1-ones including 2-aryl-3-(2,5-dihydroxyphenyl)cyclopent-2-ene-1-ones (2a-2f) and 3-aryl-2-3',4',5'-trimethoxyphenyl)cyclopent-2-ene-1-one (3a-3j) were synthesized and evaluated for the cytotoxicity against three tumor cell lines; B16F10, HCT116 and A431. It was found that the 3,4,5-trimethoxy substituent was optimal for the bioactivity of compounds in series 2. Meanwhile, compounds in series 3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound 3f), (3-hydroxy-4-methoxy)phenyl (compound 3e), or (3-amino-4-methoxy)phenyl (compound 3j).

Animals↗
PubMed2002

Molecular cloning and phylogenetic analysis of new human endogenous retrovirus HERV-W family in cancer cells.

A human endogenous retroviral family (HERV-W) has recently been described that is related to multiple sclerosis-associated retrovirus (MSRV) sequences. By using the PCR approach with human genomic DNA derived from cancer cell lines (HepG2, Jurkat, MCF7, UO-31), five env fragments of HERV-W family were newly identified and analyzed. They showed a high degree of nucleotide sequence similarity (94-99%) with that of the HERV-W. Translation of the env fragments showed no frameshift and termination codon by deletion/insertion or point mutation in clones HepG2-1 and JUR-3. The ratio of synonymous to non-synonymous substitutions indicated that negative selective pressure is acting on HepG2-1 and JUR-3 sequences. These env gene sequences could be associated with an active provirus in human cancer cells (HepG2 and Jurkat). The HepG2-1 and JUR-3 showed sister relationship with the HERV-W and W-7-1 derived from human Chromosome (Chr) 7. Phylogenetic analysis from the HERV-W family indicated close relationships of the env gene sequences across human chromosomes.

Amino Acid Substitution↗