|Description||Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I). It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drugs. It was isolated from the bark and stem of Camptotheca acuminata (Camptotheca, Happy tree), a tree native to China used as a cancer treatment in Traditional Chinese Medicine. CPT showed remarkable anticancer activity in preliminary clinical trials but also low solubility and (high) adverse drug reaction. Because of these disadvantages synthetic and medicinal chemists have developed numerous syntheses of Camptothecin and various derivatives to increase the benefits of the chemical, with good results. Two CPT analogues have been approved and are used in cancer chemotherapy today, topotecan and irinotecan|
For comparison purposes, the ADC A1 -mc-MMAD and/or A1 -vc-MMAD were used. The linker payload, mc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) was conjugate...
Auristatin F is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAF analog and cytotoxin in Antibody-drug conjugates.
Taltobulin (formerly HTI-286) is a fully synthetic analog of the natural tripeptide hemiasterlin, inhibits tubulin polymerization and circumvents transport-base...
MMAD is a highly potent inhibitor of tubulin.
Dolastatin 10 is an inhibitior of microtubule disassembly (IC50= 1.2μM) and potently inhibits vincristine binding to tubulin in a noncompetitive manner ( Ki= 1....
After an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) ...
Daunomycin is an important anti-tumor agent, mainly used in the treatment of acute leukemias. Daunomycin can inhibit DNA synthesis by the way of binding to DNA(...
MMAE, whose full name is Monomethyl auristatin E, inhibits tubulin polymerization so that it inhibits cell division.
HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in ...
The cytotoxicity of PNU-159682 were in the subnanomolar range (0.07-0.58 nmol/L) and noticeably lower than that recorded for both MMDX and doxorubicin; PNU-1596...
Ansamitocin P-3, a potent anti-tumor maytansinoid found in Actinosynnema pretiosum, is a maytansine analog which displays potent cytotoxicity against the human ...
Maytansinol disrupts the mitotic spindle and prevents mitotic exit in Drosophila used in the preparation of site-specific trastuzumab maytansinoid antibody-drug...
Triptolide is a diterpenoid epoxide found in the Thunder God Vine, Tripterygium wilfordii, which has been used in traditional Chinese medicine for more than two...
Doxorubicin is an anthracycline antibiotic with antineoplastic activity. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the hy...
Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis. It is a drug used in cancer chemotherap...
Ansamitocin P-3, a metabolite of Ansamitocin, displays potent cytotoxicity against as a a new maytansinoid antitumor antibiotic.
Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative with improved pharmacological features and higher water solubility. It induced mitotic cell cycle ar...
Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I). It was discovered in 1966 by M. E. Wall and M. C. W...
Calicheamicin, also known as Calichemicin γ1, is an potent enediyne antitumor antibiotics derived from the bacterium Micromonospora echinospora. Calicheamicin t...