Antitumoral activity of 1,2-diaminocyclohexane derivatives in breast, colon and skin human cancer cells.
Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities against the MCF-7, HCT-116 and A375 cancer cell lines. Cell cycle and apoptosis analyses were also carried out. Our results show that all the compounds are potent cytotoxic agents, especially against the A375 cell line.



The selective activity of the macrocyclic derivative against A375, via apoptosis, supposes a great advantage for future therapeutic use. This exemplifies the potential of 1,2-diaminocyclohexane derivatives to qualify as lead structures for future anticancer drug development due to their easy syntheses and noteworthy bioactivity.
Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Granada 18071, Spain.
Fátima
F
Morales
Instituto de Biopatología y Medicina Regenerativa (IBIMER), Departamento de Anatomía y Embriología Humana, Facultad de Medicina, Granada 18071, Spain.|Departamento de Ciencias de la Salud, Facultad de Ciencias Experimentales y de la Salud, Jaén 23071, Spain.
Alberto
A
Ramírez
Instituto de Biopatología y Medicina Regenerativa (IBIMER), Departamento de Anatomía y Embriología Humana, Facultad de Medicina, Granada 18071, Spain.|Instituto Biosanitario de Granada (ibs.GRANADA), Hospitales Universitarios de Granada-Universidad de Granada, Granada 18071, Spain.
Cynthia
C
Morata-Tarifa
Instituto de Biopatología y Medicina Regenerativa (IBIMER), Departamento de Anatomía y Embriología Humana, Facultad de Medicina, Granada 18071, Spain.|Instituto Biosanitario de Granada (ibs.GRANADA), Hospitales Universitarios de Granada-Universidad de Granada, Granada 18071, Spain.
Saúl A
SA
Navarro
Instituto de Biopatología y Medicina Regenerativa (IBIMER), Departamento de Anatomía y Embriología Humana, Facultad de Medicina, Granada 18071, Spain.|Instituto Biosanitario de Granada (ibs.GRANADA), Hospitales Universitarios de Granada-Universidad de Granada, Granada 18071, Spain.
Juan A
JA
Marchal
Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Granada 18071, Spain.|Instituto Biosanitario de Granada (ibs.GRANADA), Hospitales Universitarios de Granada-Universidad de Granada, Granada 18071, Spain.
Joaquín M
JM
Campos
Departamento de Química Farmacéutica y Orgánica, Facultad de Farmacia, Granada 18071, Spain.|Instituto Biosanitario de Granada (ibs.GRANADA), Hospitales Universitarios de Granada-Universidad de Granada, Granada 18071, Spain.
Ana
A
Conejo-García
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D017209:Apoptosis; D001943:Breast Neoplasms; D002453:Cell Cycle; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D003110:Colonic Neoplasms; D003514:Cyclohexylamines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D012878:Skin Neoplasms; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D003514:Cyclohexylamines; C030435:1,2-cyclohexanediamine
1; 2-diaminocyclohexanes; antitumor; apoptosis; benzenesulfonamides; breast cancer; caspases; colon cancer; macrocycles; melanoma