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Newly acylated SN-38 homodimers: carrier-free nano-prodrugs for chemotherapy

Sanjay Kumar 1
Sanjay Kumar
, 
Yoshitaka Koseki 1
Yoshitaka Koseki
, 
Keita Tanita 1
Keita Tanita
, 
Hitoshi Kasai 1
Hitoshi Kasai
1 Institute of Multidisciplinary Research for Advanced Materials, Tohoku University, Sendai, Miyagi 980-8577, Japan
10.71267/mencom.7664
Published 2025-03-31
Communication , Volume 35, Issue 3, 278-281
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Kumar S. et al. Newly acylated SN-38 homodimers: carrier-free nano-prodrugs for chemotherapy // Mendeleev Communications. 2025. Vol. 35. No. 3. pp. 278-281.
GOST all authors (up to 50) Copy
Kumar S., Koseki Y., Tanita K., Kasai H. Newly acylated SN-38 homodimers: carrier-free nano-prodrugs for chemotherapy // Mendeleev Communications. 2025. Vol. 35. No. 3. pp. 278-281.
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TY - JOUR
DO - 10.71267/mencom.7664
UR - https://mendcomm.colab.ws/publications/10.71267/mencom.7664
TI - Newly acylated SN-38 homodimers: carrier-free nano-prodrugs for chemotherapy
T2 - Mendeleev Communications
AU - Kumar, Sanjay
AU - Koseki, Yoshitaka
AU - Tanita, Keita
AU - Kasai, Hitoshi
PY - 2025
DA - 2025/03/31
PB - Mendeleev Communications
SP - 278-281
IS - 3
VL - 35
ER -
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@article{2025_Kumar,
author = {Sanjay Kumar and Yoshitaka Koseki and Keita Tanita and Hitoshi Kasai},
title = {Newly acylated SN-38 homodimers: carrier-free nano-prodrugs for chemotherapy},
journal = {Mendeleev Communications},
year = {2025},
volume = {35},
publisher = {Mendeleev Communications},
month = {Mar},
url = {https://mendcomm.colab.ws/publications/10.71267/mencom.7664},
number = {3},
pages = {278--281},
doi = {10.71267/mencom.7664}
}
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Kumar, Sanjay, et al. “Newly acylated SN-38 homodimers: carrier-free nano-prodrugs for chemotherapy.” Mendeleev Communications, vol. 35, no. 3, Mar. 2025, pp. 278-281. https://mendcomm.colab.ws/publications/10.71267/mencom.7664.
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Keywords

7-ethyl-10-hydroxycamptothecin
anticancer
carrier-free
disulfides
irinotecan
nano-prodrug
organic carbonates
SN-38 C5 dimer

Abstract

Homodimers based on 7-ethyl-10-hydroxycamptothecin (SN-38) containing S2[(CH2)2OC(O)]2 bridge and acyl substituents were synthesized and used for fabrication of nano-prodrugs. The latter demonstrated remarkable dispersion and stability over one month when stored at a temperature of 4 °C, with an ideal size of nanoparticles in the range of 80–130 nm that is required for EPR effect. The homodimer containing cyclopropylacetyl substituent chain exhibited significant anticancer efficacy against the HCT-116 and A-549 cell lines, with IC50 values having been 0.07 ± 0.01 and 0.29 ± 0.02 μm, respectively.

Funders

Ministry of Education, Culture, Sports, Science, and Technology in Japan
22F22102 (H.K.)

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