RT Journal Article
T1 3D-Printing of Capsule Devices as Compartmentalization Tools for Supported Reagents in the Search of Antiproliferative Isatins
A1 Malatini, Camilla
A1 Carbajales, Carlos
A1 Luna, Mariángel
A1 Beltrán, Osvaldo
A1 Amorín López, Manuel
A1 Fernández Masaguer, Jorge Christian
A1 Blanco Fernández, José Manuel
A1 Barbosa Fernández, Silvia
A1 Taboada Antelo, Pablo
A1 Coelho Cotón, Alberto José
K1 3D printing
K1 Catalyst compartmentation
K1 Polypropylene capsule
K1 Supported reagents
K1 Isatins
K1 Anticancer
AB The application of high throughput synthesis methodologies in the generation of active pharmaceutical ingredients (APIs) currently requires the use of automated and easily scalable systems, easy dispensing of supported reagents in solution phase organic synthesis (SPOS), and elimination of purification and extraction steps. The recyclability and recoverability of supported reagents and/or catalysts in a rapid and individualized manner is a challenge in the pharmaceutical industry. This objective can be achieved through a suitable compartmentalization of these pulverulent reagents in suitable devices for it. This work deals with the use of customized polypropylene permeable-capsule devices manufactured by 3D printing, using the fused deposition modeling (FDM) technique, adaptable to any type of flask or reactor. The capsules fabricated in this work were easily loaded “in one step” with polymeric reagents for use as scavengers of isocyanides in the work-up process of Ugi multicomponent reactions or as compartmentalized and reusable catalysts in copper-catalyzed cycloadditions (CuAAC) or Heck palladium catalyzed cross-coupling reactions (PCCCRs). The reaction products are different series of diversely substituted isatins, which were tested in cancerous cervical HeLa and murine 3T3 Balb fibroblast cells, obtaining potent antiproliferative activity. This work demonstrates the applicability of 3D printing in chemical processes to obtain anticancer APIs.
PB MDPI
SN 1424-8247
YR 2023
FD 2023-02-16
LK https://hdl.handle.net/10347/38301
UL https://hdl.handle.net/10347/38301
LA eng
NO Malatini, C.; Carbajales, C.; Luna, M.; Beltrán, O.; Amorín, M.; Masaguer, C.F.; Blanco, J.M.; Barbosa, S.; Taboada, P.; Coelho, A. 3D-Printing of Capsule Devices as Compartmentalization Tools for Supported Reagents in the Search of Antiproliferative Isatins. Pharmaceuticals 2023, 16, 310. https://doi.org/10.3390/ph16020310
NO This research was funded by the Agencia Estatal de Investigación (AEI), project number PID2019–109517RB-I00 and the Xunta de Galicia ED431C 2022/18. ERDF funds are also acknowledged. This work was also financially supported by the Consellería de Cultura, Educación e Ordenación Universitaria of the Galician Government: EM2014/022 to A.C. M.A. thanks Xunta de Galicia and the ERDF (ED431C 2021/21).
DS Minerva
RD 24 abr 2026