ABSTRACT
A series of dehydroepiandrosterone derivatives containing an acid ester was synthesized and evaluated for their antitumor activity on ES-2, A549, and HepG2 cells by the MTT assay. Most compounds showed antitumor activity, while compounds 1c, 2i, and 2o exhibited more potential inhibitory effects compared with dehydroepiandrosterone on ES-2 cells, A549 cells, and HepG2 cells, respectively.
Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Dehydroepiandrosterone/analogs & derivatives , Dehydroepiandrosterone/pharmacology , Antineoplastic Agents/chemical synthesis , Cell Line, Tumor , Cell Survival/drug effects , Dehydroepiandrosterone/chemical synthesis , Drug Screening Assays, Antitumor , Hep G2 Cells , Humans , Neoplasms/drug therapyABSTRACT
36 Novel heterocyclic chalcone derivatives were synthesized and tested for their anti-bacterial activity. Some compounds presented good anti-microbial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). This class of compounds presented high potency against Streptococcus mutans, among which the derivatives F2 with an MIC of 2 µg/mL was as active as the standard drug (norfloxacin) and less active than oxacillin. All the compounds did not inhibit the growth of Gram-negative bacteria (Escherichia coli CCARM 1924 or Escherichia coli CCARM 1356) at 64 µg/mL.
Subject(s)
Anti-Bacterial Agents/chemical synthesis , Chalcone/analogs & derivatives , Chalcone/chemical synthesis , Drug Design , Furans/chemistry , Quinolines/chemistry , Sulfur Compounds/chemistry , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Chalcone/chemistry , Chalcone/pharmacology , Drug Resistance, Multiple, Bacterial/drug effects , Gram-Negative Bacteria/drug effects , Gram-Negative Bacteria/growth & development , Gram-Negative Bacteria/isolation & purification , Gram-Positive Bacteria/drug effects , Gram-Positive Bacteria/growth & development , Gram-Positive Bacteria/isolation & purification , Microbial Sensitivity Tests , Molecular StructureABSTRACT
A series of panaxadiol derivatives have been synthesized by the simple acylation of the 3-hydroxy group of panaxadiol. The anti-tumor activities of the synthesized compounds were evaluated against a panel of human tumor cell lines by the standard MTT assay. Compounds 2, 11, 12, 13, 14, 15 and 16 showed stronger antiproliferative activities than that of Rg3 and PD on the growth of the distinct cancer cell lines in vitro.
Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Ginsenosides/chemistry , Ginsenosides/pharmacology , Antineoplastic Agents/chemistry , Cell Line, Tumor , Cell Survival/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Ginsenosides/chemical synthesis , Humans , Molecular Conformation , Stereoisomerism , Structure-Activity RelationshipABSTRACT
In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)acetamides were synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume in isolated rabbit heart preparations. Some of these derivatives exhibited favorable activity compared with the standard drug, milrinone, among which 2-(4-(4-methylbenzyl)-[1,4]-diazepan-1-yl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamide (6m) was the most potent, increasing stroke volume by 8.38±0.16% (milrinone 2.45± 0.06%) at 3 x 10(-5) m. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.
Subject(s)
Acetamides , Azepines/chemical synthesis , Azepines/pharmacology , Cardiotonic Agents , Heart/drug effects , Milrinone/pharmacology , Myocardial Contraction/drug effects , Stroke Volume/drug effects , Triazoles/chemical synthesis , Triazoles/pharmacology , Acetamides/chemical synthesis , Acetamides/pharmacology , Animals , Cardiotonic Agents/chemical synthesis , Cardiotonic Agents/pharmacology , Organ Culture Techniques/methods , RabbitsABSTRACT
We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit-heart. Several compounds were developed from, and showed favorable activities compared with the standard drug milrinone. Compound 5o was the most potent with an increased stroke volume of 9.17 ± 0.14% (milrinone 2.47 ± 0.08%) at 3 × 10â»5 M in our in-vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated.
