1613697-49-6

Upstream product

• 1334524-26-3 C₆₇H₉₃NO₁₈S₂Si 
• 1334524-25-2 [2-({5-oxo-5-[(triisopropylsilyl)oxy]pentan-2-yl}disulfanyl)phenyl]acetic acid 
• 6066-82-6 1-hydroxy-pyrrolidine-2,5-dione 
• 1334524-27-4 C₅₈H₇₃NO₁₈S₂ 
• 1334524-24-1 triisopropylsilyl 4-(pyridine-2-yldisulfanyl)pentanoate 
• 452072-22-9 (±)-4-(pyridin-2-yldisulfanyl)pentanoic acid 
• 178250-23-2 ST-T-1214 
• 125791-83-5 4-mercapto-pentanoic acid 
• 108-29-2 5-methyl-dihydro-furan-2-one 

Downstream Products

• 1613697-56-5 C₈₄H₁₁₅N₁₁O₂₂S₃ 
• 1334524-28-5 C₆₆H₈₉N₅O₂₀S₂ 

Relevant academic research and scientific papers

SYNTHESIS OF NOVEL ASYMMETRIC BOW-TIE PAMAM DENDRIMER-BASED CONJUGATES FOR TUMOR-TARGETING DRUG DELIVERY

The present disclosure relates to a dendrimer-based conjugate of the formula Vm-D-C-D'-(T-F)n, which is useful for tumor targeting drug delivery. The use of asymmetric dendrimers allow for specific targeting as well as synthetic reproducibility.

THERAPEUTIC AGENT FOR TREATING TUMORS

The present disclosure relates to a therapeutic agent of the formula: Z-C(=O)-(CH2)n-?-S-S-(CRR')m-(CH2)p-C(=O)- NH-(CH2)q-NH-Y[NH-(CH2)r-X-T-W][NH-(CH2-CH-O)t (CH2)s-NH-V] Formula I or a pharmaceutically acceptable salt thereof, useful for treating tumors, including cancers. Where the compound of Formula I also contains a radionuclide or an imaging agent or both, the compound of formula I is a theranostic agent useful for treating and diagnosing tumors, including cancers.

Design, synthesis, and biological evaluations of tumor-targeting dual-warhead conjugates for a taxoid-camptothecin combination chemotherapy

Novel tumor-targeting dual-warhead conjugates, 2 (DW-1) and 3 (DW-2), which consist of a next-generation taxoid, 1 (SB-T-1214), and camptothecin as two warheads, self-immolative disulfide linkers for drug release, biotin as the tumor-targeting moiety, and 1,3,5-triazine as the tripod splitter module, were designed and synthesized. The potency of 2 was evaluated against MX-1, MCF-7, ID8, L1210FR (BR+, biotin receptor overexpressed) and WI38 (BR-, normal) cell lines in the absence and presence of glutathione (GSH), which is an endogenous thiol that triggers drug release inside the cancer cells. With the GSH and resuspension protocol, 2 exhibited IC50 values of 3.22-9.80 nM against all BR+ cancer cell lines, and 705 nM against WI38. Thus, there was a two orders of magnitude higher selectivity to cancer cells. Also, a clear cooperative effect was observed for the taxoid-camptothecin combination when two drugs were delivered to the cancer cells specifically in the form of a dual-warhead conjugate.